Title:
PREPARATION METHOD FOR 4-(4-AMINOPHENYL)MORPHOLIN-3-ONE
Document Type and Number:
WIPO Patent Application WO/2020/019529
Kind Code:
A1
Abstract:
The present invention relates to a preparation method for 4-(4-aminophenyl) morpholin-3-one. Said method comprises: using p-nitroaniline as a raw material, successively performing an amidation reaction and a catalytic hydrogenation reaction to obtain a p-acyl-substituted aminophenylamin, and then sequentially performing an amidation reaction, a halogenation reaction or a sulfonylation reaction with 1,4-dioxane-2-one to prepare N-(2-substituted ethyloxyacetyl) p-acyl-substituted aminophenylamin, performing a condensation cyclization reaction under the action of a base to obtain 4-(4-substituted acylaminophenyl) morpholin-3-one, and finally removing an acyl protecting group, so as to obtain a target product. The raw materials used in the present invention are cheap and easy to obtain. The method of the present invention is easy to operate, and has low cost. The reactions involved in each step have high activity and specificity, and are easy to carry out, and the products have high purity and high yield.
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Inventors:
LIU YUESHENG (CN)
QI YUXIN (CN)
CHEN JUN (CN)
PAN BINGCHEN (CN)
QIAN YUFENG (CN)
QI YUXIN (CN)
CHEN JUN (CN)
PAN BINGCHEN (CN)
QIAN YUFENG (CN)
Application Number:
PCT/CN2018/109953
Publication Date:
January 30, 2020
Filing Date:
October 12, 2018
Export Citation:
Assignee:
XIN FA PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D265/32; C07C231/02; C07C235/16
Foreign References:
| CN104211654A | 2014-12-17 | |||
| US3092630A | 1963-06-04 | |||
| CN104098525A | 2014-10-15 | |||
| JP2011213866A | 2011-10-27 | |||
| CN105111163A | 2015-12-02 |
Other References:
GUO, WUSHENG ET AL.: "Metal-Free Synthesis of N-Aryl Amides using Organocatalytic Ring- Opening Aminolysis of Lactones", CHEMSUSCHEM, vol. 10, no. 9, 13 April 2017 (2017-04-13), pages 1969 - 1975, XP055681519
Attorney, Agent or Firm:
JINAN JINDI INTELLECTUAL PROPERTY AGENCY CO., LTD (CN)
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